Targeted protein degradation via intramolecular bivalent glues.

Bromodomain Containing Proteins / metabolism Cell Cycle Proteins / metabolism Drug Design Proteasome Endopeptidase Complex / metabolism Proteolysis Proteolysis Targeting Chimera Transcription Factors / metabolism Ubiquitin-Protein Ligases / metabolism Ubiquitination Protein Binding Substrate Specificity Protein Domains

Journal

Nature

ISSN: 1476-4687

Titre abrégé: Nature

Pays: England

ID NLM: 0410462

Informations de publication

Date de publication:
Mar 2024

Historique:

received: 18 02 2023

accepted: 18 01 2024

medline: 8 3 2024

pubmed: 22 2 2024

entrez: 21 2 2024

Statut: ppublish

Résumé

Targeted protein degradation is a pharmacological modality that is based on the induced proximity of an E3 ubiquitin ligase and a target protein to promote target ubiquitination and proteasomal degradation. This has been achieved either via proteolysis-targeting chimeras (PROTACs)-bifunctional compounds composed of two separate moieties that individually bind the target and E3 ligase, or via molecular glues that monovalently bind either the ligase or the target

Identifiants

DOI: 10.1038/s41586-024-07089-6 PMID: 38383787 PMC: PMC10917667

pubmed: 38383787

doi: 10.1038/s41586-024-07089-6

pii: 10.1038/s41586-024-07089-6

pmc: PMC10917667

doi:

Substances chimiques

Bromodomain Containing Proteins 0

Cell Cycle Proteins 0

Proteasome Endopeptidase Complex EC 3.4.25.1

Proteolysis Targeting Chimera 0

Transcription Factors 0

Ubiquitin-Protein Ligases EC 2.3.2.27

Types de publication

Journal Article

Langues

eng

Sous-ensembles de citation

Pagination

204-211

Subventions

Organisme : Wellcome Trust

Pays : United Kingdom

Informations de copyright

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